生物活性

Purmorphamine, a purine derivative, is a Hedgehog agonist. Purmorphamine directly binds to and activates the 7-transmembrane Smo receptor of the Hedgehog signaling pathway. Hedgehog agonist Purmorphamine most significantly increased the neuronal differentiation of a human striatal NSC line (STROC05). Purmorphamine up-regulated gene expression of the mediators of Hh pathway, SMO, PTCH1, GLI1, and GLI2. The activation of Hh pathway by Purmorphamine increased the expression of several genes. Purmorphamine triggers Hh signaling pathway in hMSCs, inducing an increase in the expression of a set of genes involved in the osteoblast differentiation program. The EC50 value for differentiation of C3H10T1/2 cells based on alkaline phosphatase expression is 1 μM.

体外研究

体内研究

激酶实验

细胞实验

0.5-10 μM

动物实验

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Sinha S, et al. Nat Chem Biol, 2006, 2(1), 29-30.
[2] Beachy, Philip A., et al., 2004. Tissue repair and stem cell renewal in carcinogenesis. Nature. 432(7015): 324-31.
[3] Beloti, Márcio M., et al., 2005. Purmorphamine enhances osteogenic activity of human osteoblasts derived from bone marrow mesenchymal cells. Cell biology international. 29(7): 537-41.
[4] Wu, Xu., et al., 2004. Purmorphamine induces osteogenesis by activation of the hedgehog signaling pathway. Chemistry & biology. 11(9): 1229-38.

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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